Assay Detail
Binding
CHEMBL885593
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Displacement of [3H]5-HT from human cloned 5HT1D receptor expressed in CHO cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.31 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL241463 | — | — | 1 | 9.40 |
| CHEMBL241503 | — | — | 1 | 9.10 |
| CHEMBL183460 | — | — | 1 | 8.80 |
| CHEMBL391033 | — | — | 1 | 8.60 |
| CHEMBL239168 | — | — | 1 | 8.50 |
| CHEMBL241500 | — | — | 1 | 7.20 |
| CHEMBL241499 | — | — | 1 | 7.10 |
| CHEMBL238730 | — | — | 1 | 7.10 |
| CHEMBL393539 | — | — | 1 | 7.00 |
| CHEMBL239167 | — | — | 1 | 6.60 |
| CHEMBL238520 | — | — | 1 | 6.60 |
| CHEMBL442087 | — | — | 1 | 6.40 |
| CHEMBL238732 | — | — | 1 | 6.20 |
| CHEMBL238519 | — | — | 1 | 6.20 |
| CHEMBL239166 | — | — | 1 | 6.10 |
| CHEMBL391661 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL241463 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL241503 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL183460 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL391033 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL239168 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL241500 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL241499 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL238730 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL393539 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL239167 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL238520 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL442087 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL238732 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL238519 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL239166 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL391661 | — | Ki | = | 794.33 | nM | 6.10 |